title: Design and synthesis of orally bioavailable benzimidazoles as Raf kinase inhibitors.
abstract: A series of arylaminobenzimidazoles was designed and synthesized as Raf kinase inhibitors. Exploration of the structure-activity relationship resulted in compounds that are potent in vitro and show desirable in vivo properties.
authors.affiliation: Novartis Institutes for Biomedical Research, 4560 Horton Street, Emeryville, California 94608, USA. savithri.ramurthy@novartis.com
authors.forename: Savithri
authors.initials: S
authors.lastname: Ramurthy
authors.forename: Sharadha
authors.initials: S
authors.lastname: Subramanian
authors.forename: Mina
authors.initials: M
authors.lastname: Aikawa
authors.forename: Payman
authors.initials: P
authors.lastname: Amiri
authors.forename: Abran
authors.initials: A
authors.lastname: Costales
authors.forename: Jeff
authors.initials: J
authors.lastname: Dove
authors.forename: Susan
authors.initials: S
authors.lastname: Fong
authors.forename: Johanna M
authors.initials: JM
authors.lastname: Jansen
authors.forename: Barry
authors.initials: B
authors.lastname: Levine
authors.forename: Sylvia
authors.initials: S
authors.lastname: Ma
authors.forename: Christopher M
authors.initials: CM
authors.lastname: McBride
authors.forename: Jonah
authors.initials: J
authors.lastname: Michaelian
authors.forename: Teresa
authors.initials: T
authors.lastname: Pick
authors.forename: Daniel J
authors.initials: DJ
authors.lastname: Poon
authors.forename: Sandhya
authors.initials: S
authors.lastname: Girish
authors.forename: Cynthia M
authors.initials: CM
authors.lastname: Shafer
authors.forename: Darrin
authors.initials: D
authors.lastname: Stuart
authors.forename: Leonard
authors.initials: L
authors.lastname: Sung
authors.forename: Paul A
authors.initials: PA
authors.lastname: Renhowe
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001562:Benzimidazoles / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001682:Biological Availability; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018360:Crystallography, X-Ray; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D005260:Female; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017434:Protein Structure, Tertiary; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D023041:Xenograft Model Antitumor Assays; D048490:raf Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D001562:Benzimidazoles; D047428:Protein Kinase Inhibitors; D048490:raf Kinases